Imperial College London
Alternate

ProfessorRobertGlen

Faculty of Medicine, Department of Metabolism, Digestion and Reproduction

Chair in Computational Medicine
 
 
 
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Contact

 

+44 (0)20 7594 7912r.glen Website

 
 
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Location

 

362Sir Alexander Fleming BuildingSouth Kensington Campus

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Summary

 

Publications

Citation

BibTex format

@article{Read:2019:10.1124/pr.119.017533,
author = {Read, C and Nyimanu, D and Williams, TL and Huggins, DJ and Sulentic, P and Macrae, RGC and Yang, P and Glen, RC and Maguire, JJ and Davenport, AP},
doi = {10.1124/pr.119.017533},
journal = {Pharmacological Reviews},
pages = {467--502},
title = {International union of basic and clinical pharmacology. CVII. structure and pharmacology of the apelin receptor with a recommendation that elabela/toddler is a second endogenous peptide ligand},
url = {http://dx.doi.org/10.1124/pr.119.017533},
volume = {71},
year = {2019}
}
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RIS format (EndNote, RefMan)

TY  - JOUR
AB  - The predicted protein encoded by the APJ gene discovered in 1993 was originally classified as a class A G protein-coupled orphan receptor but was subsequently paired with a novel peptide ligand, apelin-36 in 1998. Substantial research identified a family of shorter peptides activating the apelin receptor, including apelin-17, apelin-13, and [Pyr1]apelin-13, with the latter peptide predominating in human plasma and cardiovascular system. A range of pharmacological tools have been developed, including radiolabeled ligands, analogs with improved plasma stability, peptides, and small molecules including biased agonists and antagonists, leading to the recommendation that the APJ gene be renamed APLNR and encode the apelin receptor protein. Recently, a second endogenous ligand has been identified and called Elabela/Toddler, a 54-amino acid peptide originally identified in the genomes of fish and humans but misclassified as noncoding. This precursor is also able to be cleaved to shorter sequences (32, 21, and 11 amino acids), and all are able to activate the apelin receptor and are blocked by apelin receptor antagonists. This review summarizes the pharmacology of these ligands and the apelin receptor, highlights the emerging physiologic and pathophysiological roles in a number of diseases, and recommends that Elabela/Toddler is a second endogenous peptide ligand of the apelin receptor protein.
AU  - Read,C
AU  - Nyimanu,D
AU  - Williams,TL
AU  - Huggins,DJ
AU  - Sulentic,P
AU  - Macrae,RGC
AU  - Yang,P
AU  - Glen,RC
AU  - Maguire,JJ
AU  - Davenport,AP
DO  - 10.1124/pr.119.017533
EP  - 502
PY  - 2019///
SN  - 0031-6997
SP  - 467
TI  - International union of basic and clinical pharmacology. CVII. structure and pharmacology of the apelin receptor with a recommendation that elabela/toddler is a second endogenous peptide ligand
T2  - Pharmacological Reviews
UR  - http://dx.doi.org/10.1124/pr.119.017533
UR  - http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:000500540700002&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=1ba7043ffcc86c417c072aa74d649202
UR  - http://pharmrev.aspetjournals.org/content/71/4/467
UR  - http://hdl.handle.net/10044/1/79187
VL  - 71
ER  -
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